AP521

AP521 is an agonist of human 5-HT_1A receptor with an IC₅₀ of 94 nM. IC50 & Target: IC50: 94 nM (5-HT_1A (human))^[1] In Vitro: AP521 is an agonist of human 5-HT_1A receptor with IC₅₀s of 135, 94, 254, 5530, 418, 422 and 198 nM for 5-HT_1A (rat), 5-HT_1A (human), 5-HT_1B (rat), 5-HT_1B (human), 5-HT_1D (human), 5-HT_5a (human) and 5-HT₇ (rat), respectively. AP521 also decreases the forskolin-induced cAMP accumulation from 10 nM to 10 μM^[1]. In Vivo: AP521 significantly increases the number of shock acceptances [F(5,105)=4.46, P<0.01] at doses between 0.5 to 10 mg/kg. Oral administration of AP521 at 3 and 10 mg/kg significantly decreases freezing time [F(3,60)=2.89, P<0.05]. AP521 significantly increases the time spent on the open arms by approximately 2-fold as compare to the vehicle treated group [F(3, 36)=4.21, P<0.05 for AP521]. The anxiolytic-like effect of AP521 appears to be dose-related. AP521 significantly increases the extracellular 5-HT level of the medial prefrontal cortex (mPFC) at 10 mg/kg from 0.5 to 1 h after administration. AP521 at 3 mg/kg tends to increase the extracellular 5-HT level, however, this increase is not significant^[1].